Absztrakt In the frame of our diversity-oriented research on multitarget small molecule anticancer agents, utilizing convergent synthetic sequences terminated by Sonogashira coupling reactions, a preliminary selection of representative alkyne-tethered vindoline hybrids was synthesized. The novel hybrids with additional pharmacophoric fragments…
Absztrakt A series of novel vindoline–piperazine conjugates were synthesized by coupling 6 N-substituted piperazine pharmacophores at positions 10 and 17 of Vinca alkaloid monomer vindoline through different types of linkers. The in vitro antiproliferative activity of the 17 new conjugates was investigated on…
Absztrakt Replacing fossil fuels with renewable, bio-based alternatives is inevitable for the modern chemical industry, in line with the 12 principles of green chemistry. 2,5-Furandicarboxylic acid (FDCA) is a promising platform molecule that can be derived from 5-hydroxymethyl furfural (HMF)…
Absztrakt In the pursuit of circular economies aimed at eliminating waste and pollution, chemical recycling emerges as a promising avenue for transforming plastics into monomers. This study addresses the need for economically viable and mild depolymerisation methods, focusing on poly(bisphenol…
Absztrakt A lipase from Burkholderia cepacia was covalently linked to the surface of Laponite® layered silicate after its activation with glycidoxy moieties on two different routes. The modified silicate was embedded into poly-ε-caprolacton (PCL) for the preparation of self-degradable biopolymers. The activated…
Absztrakt Human tyrosine hydroxylase (hTH) has key role in the production of catecholamine neurotransmitters. The structure, function and regulation of hTH has been extensively researched area and the possibility of enzyme replacement therapy (ERT) involving hTH through nanocarriers has been raised as well. However, our understanding on how…
Absztrakt β-Aminophosphonates obtained by the Michael addition of primary amines to the double bond of diethyl vinylphosphonate proved to be suitable starting materials (amine components) in the Kabachnik–Fields reaction with formaldehyde and dialkyl phosphites or secondary phosphine oxides to afford N-phosphonylmethyl-…
Absztrakt The synthesis of potentially biologically active phosphinoyl functionalized N-(2-(phenylethynyl)benzyl)amine, 1,2-dihydro-isoquinoline and 2H-isoindoline via a multicomponent reaction of 2-(phenylethynyl)benzaldehyde, amine and diphenylphosphine oxide is described for the first time. Depending on the catalyst and the conditions used, the same one-pot three-component reaction can…
Absztrakt Capsaicin and its derivatives are special alkaloids responsible for the pungency of spicy pepper fruits and are mainly used in the pharmaceutical, food, and cosmetic industries. Until now, only batch syntheses of capsaicin and some of its analogues have…
Absztrakt Exenatide (Ex4), a GLP-1 incretin mimetic polypeptide, is an effective therapeutic agent against diabetes and obesity. We highlight the indirect role of Ex4’s structure-stabilizing Trp-cage (Tc) motif in governing GLP-1 receptor (GLP-1R) signal transduction. We use various Ex4 derivatives…